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Ureases have been emerged as significant virulence factors implicated in the pathogenesis of many clinical conditions such as pyelonephritis, hepatic coma, peptic ulceration, and the formation of injection-induced urinary stones and stomach cancer. Strategies based on urease inhibition are the main treatment of diseases caused by urease producing bacteria. The book will discuss our endeavors toward the developments of new heterocyclic compounds (triazoles & thiadiazoles) in the burgeoning field of urease inhibition in medicinal chemistry with an emphasis on the insights that have been gleaned into the structural features that contribute to high and promising levels of anti-urease activity. Antioxidant potential and antibacterial efficacy of the represented structural leads further open up the opportunities to contribute toward the health-protecting factors.